Emerging therapies in the treatment of 'diabesity': Beyond GLP-1

Trends in Pharmacological Sciences

Volumn 32, Issue 1, 2011, Pages 8-15

  Tharakan, George ^a   Tan, Tricia ^a   Bloom, Stephen ^a  

^a IMPERIAL COLLEGE LONDON   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

AMYLIN; ANTIDIABETIC AGENT; ANTIOBESITY AGENT; BYDUREON; DIPEPTIDYL PEPTIDASE IV INHIBITOR; EXENDIN 4; GASTRIC INHIBITORY POLYPEPTIDE; GASTRIC INHIBITORY POLYPEPTIDE RECEPTOR AGONIST; GASTRIC INHIBITORY POLYPEPTIDE RECEPTOR ANTAGONIST; GHRELIN; GLITAZONE DERIVATIVE; GLUCAGON; GLUCAGON LIKE PEPTIDE 1; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; GLUCAGON LIKE PEPTIDE 1 RECEPTOR AGONIST; GLUCAGON RECEPTOR AGONIST; GROWTH HORMONE SECRETAGOGUE RECEPTOR 1A ANTAGONIST; HEMOGLOBIN A1C; INSULIN GLARGINE; LIRAGLUTIDE; METFORMIN; OBESTATIN; ORAL ANTIDIABETIC AGENT; OXYNTOMODULIN; PEPTIDE YY [3-36]; PIOGLITAZONE; PLACEBO; SITAGLIPTIN; SULFONYLUREA; TASPOGLUTIDE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VILDAGLIPTIN;

BARIATRIC SURGERY; CANCER RISK; COMORBIDITY; DIABETES CONTROL; DOSAGE SCHEDULE COMPARISON; DRUG HALF LIFE; DRUG HYPERSENSITIVITY; DRUG MEGADOSE; DRUG WITHDRAWAL; ENERGY EXPENDITURE; FOOD INTAKE; GASTROINTESTINAL SYMPTOM; GLUCOSE METABOLISM; HORMONE BLOOD LEVEL; HORMONE RELEASE; HUMAN; HYPERGLYCEMIA; HYPOGLYCEMIA; INFECTION RATE; INJECTION SITE REACTION; MALABSORPTION; NAUSEA; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY; PRIORITY JOURNAL; PROTEIN SECRETION; REVIEW; SIDE EFFECT; SKIN MANIFESTATION; STOMACH BYPASS; SURGICAL TECHNIQUE; UNSPECIFIED SIDE EFFECT; VOMITING; WEIGHT GAIN; WEIGHT REDUCTION;

ANIMALS; BARIATRIC SURGERY; DIABETES MELLITUS, TYPE 2; GASTROINTESTINAL HORMONES; GHRELIN; HUMANS; MOLECULAR TARGETED THERAPY; OBESITY; RECEPTORS, GASTROINTESTINAL HORMONE; RECEPTORS, GHRELIN;

EID: 78650902671     PISSN: 01656147     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tips.2010.10.003     Document Type: Review

References (96)

1. S. Wild Global prevalence of diabetes: estimates for the year 2000 and projections for 2030 Diabetes Care 27 2004 1047 1053
2. A. Astrup, and N. Finer Redefining type 2 diabetes: 'diabesity' or 'obesity dependent diabetes mellitus'? Obes. Rev. 1 2000 57 59
3. S.E. Kahn Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy N. Engl. J. Med. 355 2006 2427 2443
4. M.F. Pollack Patient-reported tolerability issues with oral antidiabetic agents: Associations with adherence; treatment satisfaction and health-related quality of life Diabetes Res. Clin. Pract. 87 2010 204 210
5. L. Sjostrom Effects of bariatric surgery on mortality in Swedish obese subjects N. Engl. J. Med. 357 2007 741 752
6. H. Buchwald Weight and type 2 diabetes after bariatric surgery: systematic review and meta-analysis Am. J. Med. 122 2009 248-256 e245
7. H. Buchwald Bariatric surgery: a systematic review and meta-analysis JAMA 292 2004 1724 1737
8. J.P. Thaler, and D.E. Cummings Minireview: Hormonal and metabolic mechanisms of diabetes remission after gastrointestinal surgery Endocrinology 150 2009 2518 2525
9. J. Korner Exaggerated glucagon-like peptide-1 and blunted glucose-dependent insulinotropic peptide secretion are associated with Roux-en-Y gastric bypass but not adjustable gastric banding Surg. Obes. Relat. Dis. 3 2007 597 601
10. R.H. Clements Hormonal changes after Roux-en Y gastric bypass for morbid obesity and the control of type-II diabetes mellitus Am. Surg. 70 2004 1 4 discussion 4-5
11. F. Rubino The early effect of the Roux-en-Y gastric bypass on hormones involved in body weight regulation and glucose metabolism Ann. Surg. 240 2004 236 242
12. L.L. Baggio, and D.J. Drucker Biology of incretins: GLP-1 and GIP Gastroenterology 132 2007 2131 2157
13. J.F. Todd Glucagon-like peptide-1 (GLP-1): a trial of treatment in non-insulin-dependent diabetes mellitus Eur. J. Clin. Invest. 27 1997 533 536
14. R. Mentlein Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum Eur. J. Biochem. 214 1993 829 835
15. D.J. Drucker, and M.A. Nauck The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes Lancet 368 2006 1696 1705
16. D.M. Kendall Effects of exenatide (exendin-4) on glycemic control over 30 weeks in patients with type 2 diabetes treated with metformin and a sulfonylurea Diabetes Care 28 2005 1083 1091
17. B. Zinman The effect of adding exenatide to a thiazolidinedione in suboptimally controlled type 2 diabetes: a randomized trial Ann. Intern. Med. 146 2007 477 485
18. J.B. Buse Metabolic effects of two years of exenatide treatment on diabetes, obesity, and hepatic biomarkers in patients with type 2 diabetes: an interim analysis of data from the open-label, uncontrolled extension of three double-blind, placebo-controlled trials Clin. Ther. 29 2007 139 153
19. E.A. Schwartz Exenatide suppresses postprandial elevations in lipids and lipoproteins in individuals with impaired glucose tolerance and recent onset type 2 diabetes mellitus Atherosclerosis 212 2010 217 222
20. T. Okerson Effects of exenatide on systolic blood pressure in subjects with type 2 diabetes Am. J. Hypertens. 23 2010 334 339
21. J.P. Gutzwiller Glucagon-like peptide 1 induces natriuresis in healthy subjects and in insulin-resistant obese men J. Clin. Endocrinol. Metab. 89 2004 3055 3061
22. G. Xu Exendin-4 stimulates both beta-cell replication and neogenesis, resulting in increased beta-cell mass and improved glucose tolerance in diabetic rats Diabetes 48 1999 2270 2276
23. A.H. Barnett Tolerability and efficacy of exenatide and titrated insulin glargine in adult patients with type 2 diabetes previously uncontrolled with metformin or a sulfonylurea: a multinational, randomized, open-label, two-period, crossover noninferiority trial Clin. Ther. 29 2007 2333 2348
24. S.N. Davis Exploring the substitution of exenatide for insulin in patients with type 2 diabetes treated with insulin in combination with oral antidiabetes agents Diabetes Care 30 2007 2767 2772
25. M.A. Nauck A comparison of twice-daily exenatide and biphasic insulin aspart in patients with type 2 diabetes who were suboptimally controlled with sulfonylurea and metformin: a non-inferiority study Diabetologia 50 2007 259 267
26. R.J. Heine Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes: a randomized trial Ann. Intern. Med. 143 2005 559 569
27. R.A. DeFronzo Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes Diabetes Care 28 2005 1092 1100
28. K. Madsen Structure-activity and protraction relationship of long-acting glucagon-like peptide-1 derivatives: importance of fatty acid length, polarity, and bulkiness J. Med. Chem. 50 2007 6126 6132
29. J.B. Buse Liraglutide once a day versus exenatide twice a day for type 2 diabetes: a 26-week randomised, parallel-group, multinational, open-label trial (LEAD-6) Lancet 374 2009 39 47
30. L. Bjerre Knudsen Glucagon-like Peptide-1 receptor agonists activate rodent thyroid C-cells causing calcitonin release and C-cell proliferation Endocrinology 151 2010 1473 1486
31. Parks, M. and Rosebraugh, C. (2010) Weighing risks and benefits of liraglutide - the FDA's review of a new antidiabetic therapy. N. Engl. J. Med. 362, 774-777
32. I. Raz Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus Diabetologia 49 2006 2564 2571
33. B. Richter Dipeptidyl peptidase-4 (DPP-4) inhibitors for type 2 diabetes mellitus Cochrane Database Syst. Rev. 2008 CD006739
34. D. Williams-Herman Safety and tolerability of sitagliptin in clinical studies: a pooled analysis of data from 10,246 patients with type 2 diabetes BMC Endocrinol. Disord. 10 2010 7
35. U. Werner Pharmacological profile of lixisenatide: A new GLP-1 receptor agonist for the treatment of type 2 diabetes Regul. Pept. 164 2010 58 64
36. Buse, J.B., et al. (2009) DURATION-1: exenatide once weekly produces sustained glycemic control and weight loss over 52 weeks. Diabetes Care 33, 1255-1261.
37. Bergenstal, R.M., et al. (2010) Efficacy and safety of exenatide once weekly versus sitagliptin or pioglitazone as an adjunct to metformin for treatment of type 2 diabetes (DURATION-2): a randomised trial. Lancet 376, 431-439
38. Diamant, M. et al. (2010) Once weekly exenatide compared with insulin glargine titrated to target in patients with type 2 diabetes (DURATION-3): an open-label randomised trial. Lancet 375, 2234-2243
39. Ratner, R. et al. (2010) Safety and tolerability of high doses of taspoglutide, a once-weekly human GLP-1 analogue, in diabetic patients treated with metformin: a randomized double-blind placebo-controlled study. Diabet. Med. 27, 556-562
40. J. Rosenstock Potential of albiglutide, a long-acting GLP-1 receptor agonist, in type 2 diabetes: a randomized controlled trial exploring weekly, biweekly, and monthly dosing Diabetes Care 32 2009 1880 1886
41. C. Beglinger Pharmacokinetics and pharmacodynamic effects of oral GLP-1 and PYY3-36: a proof-of-concept study in healthy subjects Clin. Pharmacol. Ther. 84 2008 468 474
42. A. Flint The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans Int. J. Obes. Relat. Metab. Disord. 24 2000 288 298
43. B. Laferrere Rise of oxyntomodulin in response to oral glucose after gastric bypass surgery in patients with type 2 diabetes J. Clin. Endocrinol. Metab. 95 2010 4072 4076
44. J.J. Holst Enteroglucagon Annu. Rev. Physiol 59 1997 257 271
45. K.S. Nair Hyperglucagonemia increases resting metabolic rate in man during insulin deficiency J. Clin. Endocrinol. Metab. 64 1987 896 901
46. F.P. Alford Glucagon control of fasting glucose in man Lancet 2 1974 974 977
47. E.T. Parlevliet Oxyntomodulin ameliorates glucose intolerance in mice fed a high-fat diet Am. J. Physiol. 294 2008 E142 E147
48. K. Wynne Oxyntomodulin increases energy expenditure in addition to decreasing energy intake in overweight and obese humans: a randomised controlled trial Int. J. Obes. 30 2006 1729 1736
49. K. Wynne Subcutaneous oxyntomodulin reduces body weight in overweight and obese subjects: a double-blind, randomized, controlled trial Diabetes 54 2005 2390 2395
50. K. Hupe-Sodmann Characterisation of the processing by human neutral endopeptidase 24.11 of GLP-1(7-36) amide and comparison of the substrate specificity of the enzyme for other glucagon-like peptides Regulat. Pept. 58 1995 149 156
51. M.R. Druce Investigation of structure-activity relationships of Oxyntomodulin (Oxm) using Oxm analogs Endocrinology 150 2009 1712 1722
52. Y.L. Liu Subcutaneous oxyntomodulin analogue administration reduces body weight in lean and obese rodents Int. J. Obes. 2010 1 11
53. A. Pocai Glucagon-like peptide 1/glucagon receptor dual agonism reverses obesity in mice Diabetes 58 2009 2258 2266
54. J.W. Day A new glucagon and GLP-1 co-agonist eliminates obesity in rodents Nat. Chem. Biol. 5 2009 749 757
55. M. Kojima Ghrelin is a growth-hormone-releasing acylated peptide from stomach Nature 402 1999 656 660
56. A.M. Wren Ghrelin enhances appetite and increases food intake in humans J. Clin. Endocrinol. Metab. 86 2001 5992
57. A.M. Wren Ghrelin causes hyperphagia and obesity in rats Diabetes 50 2001 2540 2547
58. F. Broglio Ghrelin, a natural GH secretagogue produced by the stomach, induces hyperglycemia and reduces insulin secretion in humans J. Clin. Endocrinol. Metab. 86 2001 5083 5086
59. E.T. Vestergaard Ghrelin infusion in humans induces acute insulin resistance and lipolysis independent of growth hormone signaling Diabetes 57 2008 3205 3210
60. D.E. Cummings Plasma ghrelin levels after diet-induced weight loss or gastric bypass surgery N. Engl. J. Med. 346 2002 1623 1630
61. J. Korner Effects of Roux-en-Y gastric bypass surgery on fasting and postprandial concentrations of plasma ghrelin, peptide YY, and insulin J. Clin. Endocrinol. Metab. 90 2005 359 365
62. R. Peterli Improvement in glucose metabolism after bariatric surgery: comparison of laparoscopic Roux-en-Y gastric bypass and laparoscopic sleeve gastrectomy: a prospective randomized trial Ann. Surg. 250 2009 234 241
63. M. Faraj Plasma acylation-stimulating protein, adiponectin, leptin, and ghrelin before and after weight loss induced by gastric bypass surgery in morbidly obese subjects J. Clin. Endocrinol. Metab. 88 2003 1594 1602
64. C.W. Le Roux Gut hormone profiles following bariatric surgery favor an anorectic state, facilitate weight loss, and improve metabolic parameters Ann. Surg. 243 2006 108 114
65. E. Garcia-Fuentes Different effect of laparoscopic Roux-en-Y gastric bypass and open biliopancreatic diversion of Scopinaro on serum PYY and ghrelin levels Obes. Surg. 18 2008 1424 1429
66. J. Ybarra Persistent correlation of ghrelin plasma levels with body mass index both in stable weight conditions and during gastric-bypass-induced weight loss Obes. Surg. 19 2009 327 331
67. M. Sundbom Early changes in ghrelin following Roux-en-Y gastric bypass: influence of vagal nerve functionality? Obes. Surg. 17 2007 304 310
68. A. Asakawa Antagonism of ghrelin receptor reduces food intake and body weight gain in mice Gut 52 2003 947 952
69. W.P. Esler Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss Endocrinology 148 2007 5175 5185
70. L.P. Shearman Ghrelin neutralization by a ribonucleic acid-SPM ameliorates obesity in diet-induced obese mice Endocrinology 147 2006 1517 1526
71. J. Yang Inhibition of ghrelin O-acyltransferase (GOAT) by octanoylated pentapeptides Proc. Natl. Acad. Sci. U.S.A. 105 2008 10750 10755
72. O. Gualillo Introducing GOAT: a target for obesity and anti-diabetic drugs? Trends Pharmacol. Sci. 29 2008 398 401
73. J.V. Zhang Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intake Science (New York, N.Y.) 310 2005 996 999
74. C.L. Roth Ghrelin and obestatin levels in severely obese women before and after weight loss after Roux-en-Y gastric bypass surgery Obes. Surg. 19 2009 29 35
75. T.E. Adrian Human distribution and release of a putative new gut hormone, peptide YY Gastroenterology 89 1985 1070 1077
76. D.A. Keire Primary structures of PYY, [Pro(34)]PYY, and PYY-(3-36) confer different conformations and receptor selectivity Am. J. Physiol. 279 2000 G126 G131
77. R.L. Batterham Gut hormone PYY(3-36) physiologically inhibits food intake Nature 418 2002 650 654
78. R.L. Batterham Inhibition of food intake in obese subjects by peptide YY3-36 N. Engl. J. Med. 349 2003 941 948
79. R.A. Pittner Effects of PYY[3-36] in rodent models of diabetes and obesity Int. J. Obes. Relat. Metab. Disord. 28 2004 963 971
80. A.A. Ortiz A novel long-acting selective neuropeptide Y2 receptor polyethylene glycol-conjugated peptide agonist reduces food intake and body weight and improves glucose metabolism in rodents J. Pharmacol. Exp. Ther. 323 2007 692 700
81. A.M. van den Hoek PYY3-36 reinforces insulin action on glucose disposal in mice fed a high-fat diet Diabetes 53 2004 1949 1952
82. B. Sloth Effects of PYY1-36 and PYY3-36 on appetite, energy intake, energy expenditure, glucose and fat metabolism in obese and lean subjects Am. J. Physiol. Endocrinol. Metab. 292 2007 E1062 E1068
83. R.A. Pederson, and J.C. Brown The insulinotropic action of gastric inhibitory polypeptide in the perfused isolated rat pancreas Endocrinology 99 1976 780 785
84. R.A. Pederson Gastric inhibitory polypeptide, Its physiologic release and insulinotropic action in the dog Diabetes 24 1975 1050 1056
85. T. Vilsboll Reduced postprandial concentrations of intact biologically active glucagon-like peptide 1 in type 2 diabetic patients Diabetes 50 2001 609 613
86. M.A. Nauck Lack of effect of synthetic human gastric inhibitory polypeptide and glucagon-like peptide 1 [7-36 amide] infused at near-physiological concentrations on pentagastrin-stimulated gastric acid secretion in normal human subjects Digestion 52 1992 214 221
87. A. Vella, and R.A. Rizza Extrapancreatic effects of GIP and GLP-1 Horm. Metabol. Res. Hormon- und Stoffwechselforschung 36 2004 830 836
88. N. Irwin A novel, long-acting agonist of glucose-dependent insulinotropic polypeptide suitable for once-daily administration in type 2 diabetes J. Pharmacol. Exp. Ther. 314 2005 1187 1194
89. N. Irwin Comparison of the anti-diabetic effects of GIP- and GLP-1-receptor activation in obese diabetic (ob/ob) mice: studies with DPP IV resistant N-AcGIP and exendin(1-39)amide Diabetes Metab. Res. Rev. 23 2007 572 579
90. B. Gedulin Insulinotropic actions of a long acting GIP analog AC163794 in vivo 67th Scientific Sessions of the American Diabetes Association 2007
91. C.W. Chia Exogenous glucose-dependent insulinotropic polypeptide worsens post prandial hyperglycemia in type 2 diabetes Diabetes 58 2009 1342 1349
92. P.L. McClean GIP receptor antagonism reverses obesity, insulin resistance, and associated metabolic disturbances induced in mice by prolonged consumption of high-fat diet Am. J. Physiol. 293 2007 E1746 E1755
93. C.W. le Roux Supraphysiological doses of intravenous PYY3-36 cause nausea, but no additional reduction in food intake Ann. Clin. Biochem. 45 2008 93 95
94. N.M. Neary Peptide YY3-36 and glucagon-like peptide-17-36 inhibit food intake additively Endocrinology 146 2005 5120 5127
95. B.C. Field PYY3-36 and oxyntomodulin can be additive in their effect on food intake in overweight and obese humans Diabetes 59 2010 1635 1639
96. N.M. Neary No evidence of an additive inhibitory feeding effect following PP and PYY 3-36 administration Int. J. Obes. (2005) 32 2008 1438 1440